ArticleBioorganic & medicinal chemistry2009
Synthesis and antimalarial activity of new 4-amino-7-chloroquinolyl amides, sulfonamides, ureas and thioureas.
Article in Bioorganic & medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 79 citations in OpenAlex.
- Article
- Design, Synthesis and Biological Activities of (Thio)Urea Benzothiazole Derivatives.International journal of molecular sciences · 2023Review
- Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores.Molecules (Basel, Switzerland) · 2022Article
- Synthesis and Biological Importance of 2-(thio)ureabenzothiazoles.Molecules (Basel, Switzerland) · 2022Review
- A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation.Molecules (Basel, Switzerland) · 2020Article
- New peptide derived antimalaria and antimicrobial agents bearing sulphonamide moiety.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Anti-malarial effect of novel chloroquine derivatives as agents for the treatment of malaria.Malaria journal · 2017Article
- Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.Bioorganic & medicinal chemistry · 2016Article
- Design, synthesis and anticancer activity of some novel thioureido-benzenesulfonamides incorporated biologically active moieties.Chemistry Central journal · 2016Article
- Antiplasmodial activity, in vivo pharmacokinetics and anti-malarial efficacy evaluation of hydroxypyridinone hybrids in a mouse model.Malaria journal · 2015Article
- 3-Halo Chloroquine Derivatives Overcome Plasmodium falciparum Chloroquine Resistance Transporter-Mediated Drug Resistance in P. falciparum.Antimicrobial agents and chemotherapy · 2015Article
- Cytostatic versus cytocidal activities of chloroquine analogues and inhibition of hemozoin crystal growth.Antimicrobial agents and chemotherapy · 2013Article
- Antimalarial activity and mechanisms of action of two novel 4-aminoquinolines against chloroquine-resistant parasites.PloS one · 2012Article
- Design and synthesis of new N-(5-trifluoromethyl)-1H-1,2,4-triazol-3-yl benzenesulfonamides as possible antimalarial prototypes.Molecules (Basel, Switzerland) · 2011Article
- Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum.Journal of medicinal chemistry · 2010Article
- Synthesis and antimalarial activity of new chloroquine analogues carrying a multifunctional linear side chain.Bioorganic & medicinal chemistry · 2009Article
- Molecular and physiologic basis of quinoline drug resistance in Plasmodium falciparum malaria.Future microbiology · 2009Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
We report the synthesis and in vitro antimalarial activities of more than 50 7-chloro-4-aminoquinolyl-derived sulfonamides 3-8 and 11-26, ureas 19-22, thioureas 23-26, and amides 27-54. Many of the CQ analogues prepared for this study showed submicromolar antimalarial activity versus HB3 (chloroquine sensitive) and Dd2 (chloroquine resistant strains of Plasmodium falciparum) and low resistance indices were obtained in most cases. Systematic variation of the side chain length and introduction of fluorinated aliphatic and aromatic termini revealed promising leads that overcome CQ resistance. In particular, sulfonamide 3 exhibiting a short side chain with a terminal dansyl moiety combined high antiplasmodial potency with a low resistance index and showed IC(50)s of 17.5 and 22.7 nM against HB3 and Dd2 parasites.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.